RESUMO
The use of acetylation followed by silica gel column purification allowed the isolation of eight fructooligosaccharides (FOS) from the ethanol extract of Cynoglossum tubiflorus roots. Each FOS was identified by analyzing its FT-IR, HRMS/MS and NMR data, including 1H, 13C and 2D NMR HH COSY, HMBC and NOESY. In diabetic rats treated with a series of FOS from Glc-(Fru)3 to Glc-(Fru)7, a significant inhibition of intestinal α-amylase was observed. This activity increases proportionally with the FOS molecular size. It was found that they delay the absorption of total cholesterol (TC), ldl-cholesterol (LDL-C) and increase HDL-cholesterol (HDL-C) in a molecular size-dependent manner. This inhibitory effect on the activity of the digestive enzyme causes a significant (p < 0.05) reduction in the level of glucose in the blood as an anti-diabetic action. The ethanolic extract (E.E) exerts a significant effect against α-amylase as well as antihyperglycemic and antihyperlipidemic actions, while its acetylation suppresses these effects. Therefore, this study demonstrates for the first time that pure FOS act as an efficient agent in preventing hyperglycemia and hyperlipidemia and that this action evolves in the same manner with their molecular size.
Assuntos
Diabetes Mellitus Experimental , Hipoglicemiantes , Oligossacarídeos , Ratos , Animais , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Hipoglicemiantes/química , Aloxano/farmacologia , Dieta Hiperlipídica/efeitos adversos , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Espectroscopia de Infravermelho com Transformada de Fourier , Extratos Vegetais/química , Glicemia , Colesterol , alfa-AmilasesRESUMO
This study aimed to assess the biological activities of Tunisian Simmondsia chinensis and characterize their potential bioactive compounds. Different extracts of S. chinensis were tested for their antioxidant, antibacterial, anti α-amylase, and anti-acetylcholinesterase activities through in vitro assays. The methanolic extract exhibited the highest levels of antioxidant activity and total phenolic content (976.03 GAE/g extract) compared to the other extracts. Additionally, it demonstrated a substantial anti-acetylcholinesterase activity (PI= 75%) and potent antibacterial property, particularly against Enterococcus faecalis, Listeria monocytogenes, Bacillus cereus, Bacillus subtilis, and Salmonella enterica. The IC50 values of ethyl acetate and methanolic extracts against α-amylase were 42 µg/mL and 40 µg/mL, respectively, indicating potent anti-diabetic effects. HPLC-ESI-MS/MS analyses identified flavonoids and lignans as the major phenolic compounds in the methanolic extract. To better comprehend the mechanisms behind inhibitory effects on α-amylase and acetylcholinesterase enzymes, a molecular docking study was conducted. Consequently, these findings indicate that S. chinensis is a highly valuable natural resource with potential industrial applications.
RESUMO
The phytochemical investigation of Thymelaea tartonraira leaves led to the isolation and characterization of six compounds, including one new flavonoid glycoside identified as hypolaetin 8-O-ß-D-galactopyranoside (4) along with five known compounds, daphnoretin (1), triumbelletin (2), genkwanin (3), tiliroside (5) and yuankanin (6). Their structures were established based on spectroscopic methods, such as UV, IR, NMR, and HR-ESI-MS. Triumbelletin (2) and tiliroside (5) were isolated for the first time from T. tartonraira leaves. The antioxidant property of all isolated compounds was tested based on DPPH, FRAP and total antioxidant capacity assays. Compound 4 displayed an antioxidant potency more interesting than vitamin C with an IC50 =15.00±0.50â µg/ml, followed by compound 5. Furthermore, the both compounds 4 and 5 were tested for their α-amylase inhibitory activity in-vitro. Compound 4 displayed higher potency to inhibit α-amylase, with an IC50 =46.49±2.32â µg/ml, than compound 5, with an IC50 =184.2±9.2â µg/ml, while the reference compound acarbose presented the highest potency to inhibit α-amylase with an IC50 =0.44±0.022â µg/ml. Compound 4 displayed a strong inhibitory ability of α-glucosidase activity approximately twice more than the reference compound, acarbose, with IC50 values of 60.00±3.00 and 125.00±6.25â µg/ml, respectively. Thus, compound 4 exhibited a specific inhibitory activity for α-glucosidase. The molecular docking studies have supported our findings and suggested that compound 4 has been involved in various binding interactions within the active site of both enzymes α-amylase and α-glucosidase.
Assuntos
Acarbose , Flavonoides , Inibidores de Glicosídeo Hidrolases , Acarbose/análise , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo , Antioxidantes/farmacologia , Antioxidantes/análise , Flavonoides/química , Flavonoides/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Simulação de Acoplamento Molecular , Estrutura Molecular , Extratos Vegetais/química , Folhas de Planta/químicaRESUMO
This work focuses on the selection and the optimization of an efficient green-extraction method, used to recover a thymol-enriched extract from thyme (Thymus vulgaris L), as well as the evaluation of the inhibitory effect of this latter on the human platelet aggregation. Different innovative extraction techniques, namely bead milling extraction, ultrasound and microwave assisted extraction, were tested for their ability to recover a high added value extract from thyme. Among all tested eco-extraction techniques, microwave extraction (MAE) was the best method in term of its extraction yield (20.84% ± 0.51), thymol concentration (731.71 mg/g) and total phenolic (23.53 ± 1.83 mg (GAE)/g of extract) and flavonoid (6.22 ± 0.35 mg of QE/g of extract) contents. Moreover, thyme extract obtained by microwave assisted extraction (TMAE) showed the most active antioxidant effect comparing to the other tested extracts. Based on these results, TMAE was chosen to be evaluated for its antiplatelet effect. Thereby, arachidonic acid, collagen and ADP were used to induce the platelet aggregation on human platelet rich plasma taken from healthy controls and results revealed that TMAE strongly inhibited the induced platelet aggregation. Indeed, TMAE exhibited potent antiaggregant activity by inhibiting platelet activation, secretion and aggregation. Additionally, cytotoxicity assay on normal HEK-293 cells showed that TMAE has no cytotoxic effect even at high concentration (8 mg/ml) and can further be taken up to various biomedical applications mainly in the prevention of cardiovascular diseases.
Assuntos
Thymus (Planta) , Plaquetas , Células HEK293 , Humanos , Extratos Vegetais/farmacologia , Folhas de Planta , Timol/farmacologiaRESUMO
Coumarins and their derivatives are becoming a potential source for new drug discovery due to their vast array of biological activities. The present study was designed to investigate the cardioprotective effects of a newly synthesised coumarin, symbolised as 5,6-PhSHC, against cardiac remodelling process in isoproterenol (ISO) induced myocardial infarction (MI) in male Wistar rats by evaluating haematological, biochemical and cardiac biomarkers. Rats were pre/co-treated with 5,6-PhSHC or clopidogrel (150 µg/kg body weight) daily for a period of 7 days and then MI was induced by injecting ISO (85 mg/kg body weight), at an interval of 24 hours for 2 consecutive days, on the sixth and seventh days. The in vivo exploration indicated that the injection of 5,6-PhSHC improved the electrocardiographic (ECG) pattern and prevented severe heart damage by reducing leakage of the cardiac injury markers, such as troponin-T (cTn-T), lactate dehydrogenase (LDH), and creatine kinase-MB. The cellular architecture of cardiac sections, altered in the myocardium of infracted rats, was reversed by 5,6-PhSHC treatment. Results showed that injection of 5,6-PhSHC elicited significant cardioprotective effects by prevention of myocardium cell necrosis and inflammatory cells infiltration, along with marked decrease in plasma levels of fibrinogen. In addition, the total cholesterol, triglyceride, LDL-c, and HDL profiles underwent remarkable beneficial changes. It was also interesting to note that 5,6-PhSHC enhanced the antioxidative defence mechanisms by increasing myocardial glutathione (GSH) level, superoxide dismutase (SOD), and catalase (CAT) activities, together with reducing the levels of thiobarbituric-acid-reactive substances (TBARS), when compared with ISO-induced rats. Taken together, these findings suggested a beneficial role for 5,6-PhSHC against ISO-induced MI in rats. Furthermore, in silico analysis showed that 5,6-PhSHC possess high computational affinities (E-value >-9.0 kcal/mol) against cyclooxygenase-2 (PDB-ID: 1CX2), vitamin K epoxide reductase (PDB-ID: 3KP9), glycoprotein-IIb/IIIa (PDB-ID: 2VDM) and catalase (PDB-ID: 1DGF). Therefore, the present study provided promising data that the newly synthesised coumarin can be useful in the design and synthesis of novel drug against myocardial infarction.
Assuntos
Infarto do Miocárdio , Animais , Antioxidantes/metabolismo , Peso Corporal , Cardiotônicos/efeitos adversos , Catalase/metabolismo , Cumarínicos/farmacologia , Cumarínicos/uso terapêutico , Eletrocardiografia , Glutationa/metabolismo , Isoproterenol/efeitos adversos , Masculino , Infarto do Miocárdio/induzido quimicamente , Infarto do Miocárdio/tratamento farmacológico , Infarto do Miocárdio/prevenção & controle , Miocárdio/metabolismo , Estresse Oxidativo , Ratos , Ratos WistarRESUMO
The phytochemical analysis of antioxidant and antibacterial activities of Erodium arborescens aerial part extracts constitute the focus of this research. The chemical composition of an acetone extract was investigated using LC-HESI-MS2, which revealed the presence of 70 compounds. The major identified components were tannin derivatives. Total polyphenol and total flavonoid contents were assessed in plant extracts (hexane, ethyl acetate, acetone and methanol). The results showed that the acetone extract exhibited the highest contents of polyphenols and flavonoids, 895.54 and 36.39 mg QE/g DE, respectively. Furthermore, when compared to other extracts, Erodium arborescens acetone extract was endowed with the highest antioxidant activity with 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP) and total antioxidant capacity (TAC) tests. In addition, the four extracts of Erodium arborescens showed variable degrees of antimicrobial activity against the tested strains, and the interesting activity was obtained with acetone and methanol extracts.
Assuntos
Acetona , Antioxidantes , Antibacterianos/farmacologia , Antioxidantes/química , Flavonoides/química , Metanol , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polifenóis/análiseRESUMO
This study was designed to evaluate the underlying protective mechanisms of oleuropein involved in alleviating brain damage in a rat model of ischemic stroke. Male Wistar rats were divided into four groups; Control, stroke (MCAO), MCAO + clopidogrel (Clop) and MCAO + oleuropein (Ole). Results showed that the MCAO group evidenced significant brain edema (+ 9%) as well as increases of plasma cardiac markers such as lactate deshydrogenase (LDH), creatine kinase (CK-MB), fibrinogen and Trop-T by 11 %, 43%, 168 and 590%, respectively, as compared to the control group. Moreover, infarcted rats exhibited remarkable elevated levels of angiotensin converting enzyme (ACE), both in plasma and brain tissue, with astrocyte swelling and necrotic neurons in the infarct zone, hyponatremia, and increased rate of thiobarbituric acid-reactive substances (TBARS) by 89% associated with decreases in the activity of superoxide dismutase (SOD), glutathione peroxidase (GPx) and catalase (Cat) by 51%, 44 and 42%, respectively, compared to normal control rats. However, MCAO rats treated with oleuropein underwent mitigation of cerebral edema, correction of hyponatremia, remarkable decrease of plasma fibrinogen and cardiac dysfunctional enzymes, inhibition of ACE activity and improvement of oxidative stress status in brain tissue. Furthermore, in silico analysis showed considerable inhibitions of ACE, protein disulfide isomerase (PDI) and TGF-ß1, an indicative of potent anti-embolic properties. Overall, oleuropein offers a neuroprotective effect against ischemic stroke through its antioxidative and antithrombotic activities.
Assuntos
Sequestradores de Radicais Livres/uso terapêutico , Infarto da Artéria Cerebral Média/tratamento farmacológico , Glucosídeos Iridoides/uso terapêutico , Fármacos Neuroprotetores/uso terapêutico , Acetilcolinesterase/metabolismo , Animais , Encéfalo/patologia , Edema Encefálico/patologia , Edema Encefálico/prevenção & controle , Clopidogrel/uso terapêutico , Sequestradores de Radicais Livres/metabolismo , Humanos , Hiponatremia/prevenção & controle , Infarto da Artéria Cerebral Média/patologia , Glucosídeos Iridoides/metabolismo , Masculino , Simulação de Acoplamento Molecular , Fármacos Neuroprotetores/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Peptidil Dipeptidase A/metabolismo , Ligação Proteica , Isomerases de Dissulfetos de Proteínas/metabolismo , Ratos Wistar , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismoRESUMO
This study is carried out to assess the cardiopreventive effect of (E)-N'-(1-(7-methoxy-2-oxo-2H-chromen-3-yl) ethylidene)-4-methylbenzenesulfonohydrazide or SHC, a novel synthesized coumarin, against myocardial infarction induced by isoproterenol (ISO). The SHC compound was identified and characterized by spectral methods (infrared, 1 H NMR [nuclear magnetic resonance], 13 C NMR, Nuclear Overhauser Effect Spectroscopy, and high-resolution mass spectroscopy). Male Wistar rats were divided into four groups: Control, ISO (rats were injected subcutaneously by 85 mg/kg body weight [BW] of isoproterenol at Days 6 and 7 of the experience), ISO + SHC (150 µg/kg BW, orally for 7 days) and ISO + acenocoumarol (150 µg/kg BW, orally for 7 days). Results showed that ISO induced a remarkable alteration of electrocardiogram (ECG) pattern and increases of plasma cardiac troponin T, creatine kinase-MB, total cholesterol, triglycerides, low-density lipoprotein-cholesterol, lactate dehydrogenase, aspartate transaminase, and malondialdehyde. In addition, ISO reduced the high-density lipoprotein-cholesterol content and the activities of superoxide dismutase and glutathione peroxidase, with the induction of myocardial necrosis. However, SHC administration revealed a significant decrease in cardiac dysfunction markers, restored normal ECG pattern, as well as improving lipids parameters. Moreover, SHC treatment remarkably alleviated the cardiac oxidative stress and the myocardial remodeling process. Overall, the SHC offers good protection from acute myocardial infarction through the antioxidant capacity.
Assuntos
Benzenossulfonatos/farmacologia , Cardiotônicos/farmacologia , Isoproterenol/efeitos adversos , Infarto do Miocárdio , Miocárdio , Estresse Oxidativo/efeitos dos fármacos , Animais , Benzenossulfonatos/química , Cardiotônicos/química , Isoproterenol/farmacologia , Masculino , Infarto do Miocárdio/induzido quimicamente , Infarto do Miocárdio/metabolismo , Infarto do Miocárdio/patologia , Infarto do Miocárdio/prevenção & controle , Miocárdio/metabolismo , Miocárdio/patologia , Ratos , Ratos WistarRESUMO
Many species from the genus Citrus are used in traditional medicine and contain polymethoxylated flavonoids. These compounds show anti-inflammatory and chemopreventive activities, among others, and therefore have a big potential to be developed as therapeutic agents or dietary supplements. Citrus species are different in their profile and yield of polymethoxylated flavonoids. Therefore, polymethoxylated flavonoids were identified and quantified in seven different Citrus species, including wild-type and commercially available species. All species were profiled using UPLC-QTOF-MS/MS analysis combined with mass spectral molecular networking. A total of 38 polymethoxylated flavonoids were detected and 8 of them were present in every species. As the yield of polymethoxylated flavonoids was different for each species, a generally applicable HPLC-diode array detection method was developed and validated according to the ICH guidelines to quantify the amount of nobiletin and the total amount of polymethoxylated flavonoids expressed as nobiletin. Analysis of the seven samples showed evidence that wild-type Citrus species (e.g., Citrus depressa) contain higher yields of polymethoxylated flavonoids compared to commercially available species (e.g., Citrus limon). Qualitative analysis revealed the broadest variety of different PMFs in C. depressa, Citrus reticulata, and Citrus reticulata × Citrus sinensis, which makes them interesting sources of polymethoxylated flavonoids for future development as therapeutic agents or dietary supplements.
Assuntos
Citrus , Flavonoides , Extratos Vegetais/análise , Cromatografia Líquida de Alta Pressão , Citrus/química , Flavonoides/análise , Espectrometria de Massas em TandemRESUMO
Aeonium is a genus of succulents belonging to the Crassulaceae family. Their importance in traditional medicine has stimulated both pharmacological and chemical research. In this study, we optimized extraction, separation, and analytical conditions using a high performance liquid chromatographic method coupled with electrospray ionization mass spectrometry by the negative mode (HPLC-ESI-MS) in order to, for the first time, determine thirty-four compounds from Aeonium arboreum leaves. Twenty-one of them are assigned among which are sixteen flavonoids and five phenolic acids. FRAP, TAC, DPPH, and ABTSâ¢+ radical scavenging were used to evaluate antioxidant activity. The obtained IC50 values ranged from 0.031 to 0.043 mg.mL-1 for DPPH and between 0.048 and 0.09 mg·mL-1 for ABTSâ¢+. Antimicrobial activity was also assessed. The obtained minimum inhibitory concentrations (MIC) of these extracts ranged from 12.5 to 50 µg·mL-1 against Micrococcus luteus, Listeria ivanovii, Staphylococcus aureus, Salmonella enterica, Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger, and Fusarium oxysporum, and from 25 to 50 µg·mL-1 against Candida albicans. Therefore, these extracts can be considered as a potential source of biological active compounds.
Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Crassulaceae/química , Fenóis/química , Extratos Vegetais/química , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em TandemRESUMO
The strain TN638 was isolated from Tunisian soil contaminated with industrial wastewater and selected for its potent antimicrobial activity against the tested Gram positive bacteria: Staphylococcus aureus (S. aureus) ATCC 6538 and Listeria monocytogenes (L. monocytogenes) ATCCC 19117, and Gram negative bacteria: Agrobacterium tumefaciens (A. tumefaciens) ATCC 23308 and Salmonella typhimurium (S. typhimurium) ATCC 14028 and fungi: Candida albicans (C. albicans) ATCC 10231, Rhizoctonia solani (R. solani) ATCC 58938 and Fusarium sp. Solide-state fermentation (SSF) dry crude extract of the TN638 strain presents a strong inhibitory activity notably against the phytopathogenic microorganism A. tumefaciens ATCC 23308 and the two pathogenic bacteria S. aureus ATCC 6538 and L. monocytogenes ATCCC 19117 with a zone of inhibition of 48, 34 and 34 mm respectively. According to the morphological characteristic, the complete 16S rRNA gene nucleotide sequence determination [1492 bp deposited in National Center of Biotechnology Information (NCBI) database under the accession no. LN854629.1; https://www.ncbi.nlm.nih.gov/nuccore/LN854629.1/], and the phylogenetic analysis, we can deduce that our isolate is an actinomycete bacterium belonging to the genus Streptomyces and the most closely related strain was Streptomyces cavourensis (S. cavourensis) NRRL 2740T (99.9%). We propose the assignment of our strain as Streptomyces cavourensis (S. cavourensis) TN638 strain. Work-up and purification of the strain extract using different chromatographic techniques afforded seven bio-compounds namely: Cyclo-(Leu-Pro) (1), Cyclo-(Val-Pro) (2), Cyclo-(Phe-Pro) (3), nonactin (4), monactin (5), dinactin (6) and trinactin (7). The chemical structures of compounds 1-7 were confirmed by nuclear magnetic resonance (NMR) 1D and 2D spectroscopy, mass spectrometry, and comparison with literature data. The three purified diketopiperazine (DKP) derivatives (1-3), demonstrated significant antibacterial activity against A. tumefaciens ATCC 23308 and S. typhimurium ATCC 14028. The four pure macrotetrolides (4-7), exhibited strong inhibitory effect against all tested Gram positive and Gram negative bacteria notably against A. tumefaciens ATCC 23308 and S. typhimurium ATCC 14028 with a minimum inhibitory concentration (MIC) around 8 µg/mL quite similar to that of ampicillin. Thus, we propose the use of the (SSF) active extract of the S. cavourensis TN638 strain as safe biological product to control disease caused by plant pathogen A. tumefaciens. Also, the purified active molecules produced by this strain could be used in pharmaceutical field.
RESUMO
In this research work, a water-soluble polysaccharide (LAP) isolated from the fruits of Lycium arabicum was investigated. LAP contains carbohydrates (82.45±1.23 %), protein (1.56±0.21 %), and uronic acids (3.56±0.34 %). The analysis of the monosaccharide composition revealed the presence of rhamnose, arabinose, galactose, glucose and mannose in a molar ratio of 4.7 : 1.5 : 1 : 8.7 : 16.4 : 5.6. The extracted polysaccharide (PS) was considered as heterogeneous and highly branched by interpreting its GC/MS, FT-IR and NMR data. Crystallinity of LAP was inferred from its X-ray diffractometry (XRD) and Scanning Electron Microscopy (SEM) analysis. LAP exhibited an interesting stability at high temperatures (â¼254 °C) and in a wide range of pH (3-9) deduced, respectively, from its DSC and zeta potential analysis. LAP displayed a strong antioxidant activity at low concentrations evaluated by the 2,2-diphenyl-1-picrylhydrazyl (DPPH)-radical scavenging, ferric reducing activity power (FRAP), free radical scavenging ability, superoxide radical-scavenging and hydroxyl radical-scavenging abilities. Inhibition of erythrocyte hemolysis and lipid peroxidation was also assessed. In 5â h, LAP treatment allowed the protection of the damaged erythrocytes caused by AAPH (2,2-azobis(2-amidinopropane) dihydrochloride), to reduce the level of malondialdehyde (MDA) as well as to increase the reduced glutathione (GSH) level.
Assuntos
Antioxidantes/farmacologia , Eritrócitos/efeitos dos fármacos , Lycium/química , Estresse Oxidativo/efeitos dos fármacos , Polissacarídeos/farmacologia , Amidinas/toxicidade , Antioxidantes/química , Varredura Diferencial de Calorimetria , Cristalografia por Raios X , Eritrócitos/metabolismo , Glutationa/sangue , Humanos , Malondialdeído/sangue , Microscopia Eletrônica de Varredura , Polissacarídeos/química , Análise Espectral/métodosRESUMO
In the course of phytochemical and chemotaxonomical investigations of Cornulaca monacantha (Amaranthaceae), two new isoflavones, 3-(2-hydroxyphenyl)-5,7-dimethoxy-6-(methoxymethyl)-4H-1-benzopyran-4-one (1) and 7-hydroxy-3-(4-hydroxyphenyl)-5-methoxy-6-(methoxymethyl)-4H-1-benzopyran-4-one (2) were isolated from the fresh aerial parts of C. monacantha among with three known compounds named vanillic acid (3), N-cis-feruloyltyramine (4) and N-trans-feruloyltyramine (5). Their structures were elucidated by means of spectroscopic methods including one- and two-dimensional NMR and HR-ESI-MS techniques. The isolated compounds exhibited interesting antioxidant activity determined by DPPH, ABTS and TAC tests.
Assuntos
Amaranthaceae/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Isoflavonas/isolamento & purificação , Isoflavonas/farmacologia , Espectroscopia de Ressonância Magnética/métodos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Espectrometria de Massas por Ionização por Electrospray/métodosRESUMO
The chemical composition, main physicochemical properties, and biological activities of Simmondsia chinensis (S. chinensis) seeds oil were studied. The results revealed that the physiochemical characteristics of S. chinensis seeds oil were as follows: acid values 1.15 mg KOH/g, peroxide values 8.00 meq O2 Kg-1, iodine values 80.00 g/100 g of oil and saponification values 92.00 mg KOH/g, phenolic content 50.91 mg gallic acid equivalents/g extract. Gas chromatography analysis indicated that eicosenoic (55.50 %), erucic (20.43 %) and oleic (19.01 %) acids were the most abundant, saturated and unsaturated, fatty acids in the oil. Moreover, the evaluation of their antioxidant (DPPH, TAC), antibacterial, antidiabetic and acetylcholinesterase evinced interesting results. Seeds of S. chinensis constitute a substitute source for stable vegetable oil and protein with regard to nutritional and industrial applications.
Assuntos
Caryophyllales/química , Ácidos Graxos/isolamento & purificação , Extração Líquido-Líquido/métodos , Fenóis/isolamento & purificação , Óleos de Plantas/isolamento & purificação , Sementes/química , Acetilcolinesterase/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Bacillus cereus/efeitos dos fármacos , Bacillus cereus/crescimento & desenvolvimento , Bacillus subtilis/efeitos dos fármacos , Bacillus subtilis/crescimento & desenvolvimento , Compostos de Bifenilo/antagonistas & inibidores , Inibidores da Colinesterase/isolamento & purificação , Inibidores da Colinesterase/farmacologia , Enterococcus faecalis/efeitos dos fármacos , Enterococcus faecalis/crescimento & desenvolvimento , Ácidos Graxos/farmacologia , Listeria monocytogenes/efeitos dos fármacos , Listeria monocytogenes/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana , Fenóis/farmacologia , Picratos/antagonistas & inibidores , Óleos de Plantas/química , Salmonella typhimurium/efeitos dos fármacos , Salmonella typhimurium/crescimento & desenvolvimento , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/químicaRESUMO
There is a rapid increase in the percentage of elderly people in Europe. Consequently, the prevalence of age-related diseases will also significantly increase. Therefore, the main goal of MediHealth, an international research project, is to introduce a novel approach for the discovery of active agents of food plants from the Mediterranean diet and other global sources that promote healthy ageing. To achieve this goal, a series of plants from the Mediterranean diet and food plants from other origins are carefully selected and subjected to in silico, cell-based, in vivo (fly and mouse models), and metabolism analyses. Advanced analytical techniques complement the bio-evaluation process for the efficient isolation and identification of the bioactive plant constituents. Furthermore, pharmacological profiling of bioactive natural products, as well as the identification and synthesis of their metabolites, is carried out. Finally, optimization studies are performed in order to proceed to the development of innovative nutraceuticals, dietary supplements or herbal medicinal products. The project is based on an exchange of researchers between nine universities and four companies from European and non-European countries, exploiting the existing complementary multidisciplinary expertise. Herein, the unique and novel approach of this interdisciplinary project is presented.
Assuntos
Produtos Biológicos/química , Dieta Mediterrânea , Suplementos Nutricionais/análise , Envelhecimento Saudável/efeitos dos fármacos , Compostos Fitoquímicos/isolamento & purificação , Plantas Comestíveis/química , Animais , Disponibilidade Biológica , Produtos Biológicos/farmacocinética , Produtos Biológicos/farmacologia , Drosophila melanogaster/efeitos dos fármacos , Drosophila melanogaster/fisiologia , Envelhecimento Saudável/fisiologia , Humanos , Comunicação Interdisciplinar , Cooperação Internacional , Camundongos , Camundongos Endogâmicos C57BL , Ciências da Nutrição/instrumentação , Ciências da Nutrição/métodos , Compostos Fitoquímicos/química , Plantas Medicinais/químicaRESUMO
BACKGROUND: Nutritional fact study has prime importance to make the species edible and commercially viable to the food consumers. This is the first report that indicates the chemical characterization, functional, antioxidant and antihypertensive properties of Cymodocea nodosa to evaluate its nutritional status. METHODS: Physico-chemical determination was determined by colorimetric and spectroscopic analysis. The functional and texture properties were evaluated since a desirable texture should be retained. Bioactive substances were determined by liquid chromatography-high resolution electrospray ionization mass spectrometry HPLC-DAD-ESI/MS2 analysis. Health benefit of this plant was highlighting by the antioxidant and antihypertensive potentials. RESULTS: Results showed that the seagrass powder was characterized by a high content of fibers (56.4%), the fatty acids profile was dominated by the oleic acid, which represents about 62.0% of the total fatty acids and the functional properties proved important values of swelling capacity (6.71 ± 0.2) and water holding capacity (12.26 ± 0.25), that were comparable to those of some foodstuffs. Finally, the physico-chemical analysis shows the wealth in phenolic compounds, that could be explained by the high antioxidant and antihypertensive ability which was concentration dependent. CONCLUSION: The results from this study suggested that this marine plant could be utilized as a healthy food item for human consumption.
Assuntos
Alismatales/química , Inibidores da Enzima Conversora de Angiotensina/isolamento & purificação , Anti-Hipertensivos/isolamento & purificação , Antioxidantes/isolamento & purificação , Ácidos Graxos/isolamento & purificação , Alimento Funcional/análise , Fenóis/isolamento & purificação , Inibidores da Enzima Conversora de Angiotensina/química , Anti-Hipertensivos/química , Antioxidantes/química , Organismos Aquáticos , Compostos de Bifenilo/antagonistas & inibidores , Ácidos Graxos/química , Humanos , Peptidil Dipeptidase A/química , Fenóis/química , Picratos/antagonistas & inibidores , Extratos Vegetais/química , SoluçõesRESUMO
In the present study, we evaluated the antioxidant potential of Artemisia campestris essential oil (ACEO) and the possible protective effects against deltamethrin induced hepatic toxic effects. The ACEO showed radical scavenging activity with IC50 = 47.66 ± 2.51 µg/ml, ferric reducing antioxidant power (FRAP) potential (EC50 = 5.36 ± 0.77 µg/ml), superoxide scavenging activity (IC50 = 0.175 ± 0.007 µg/ml) and ËOH scavenging activity (IC50 = 0.034 ± 0.007 µg/ml). The obtained results of phenolic profile demonstrated that phenolic compounds are the major contributor to the antioxidant activity of ACEO. GC-MS analysis revealed the presence of 61 components in which monoterpene hydrocarbons constitute the major fraction (38.85%). In in vivo study, deltamethrin exposure caused an increase of serum AST, ALT and ALP activities, hepatic malondialdehyde (MDA) (measured as TBARS) and conjugated dienes markers of lipid peroxidation (LPO), while antioxidant enzyme activities (SOD, CAT and GPx) decreased significantly. Furthermore, it induces DNA damage as indicated by DNA fragmentation accompanied with severe histological changes in the liver tissues. The treatment with vitamin E or ACEO significantly improved the hepatic toxicity induced by deltamethrin. It can be concluded that vitamin E and ACEO are able to improve the hepatic oxidative damage induced by deltamethrin. Therefore, ACEO is an important product in reducing the toxic effects of deltamethrin.
Assuntos
Artemisia/química , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Doença Hepática Induzida por Substâncias e Drogas/fisiopatologia , Dano ao DNA/efeitos dos fármacos , Nitrilas/intoxicação , Óleos Voláteis/administração & dosagem , Piretrinas/intoxicação , Animais , Antioxidantes/administração & dosagem , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Citoproteção/efeitos dos fármacos , Relação Dose-Resposta a Droga , Inseticidas/intoxicação , Masculino , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Ratos , Ratos Wistar , Espécies Reativas de Oxigênio/metabolismo , Resultado do TratamentoRESUMO
This study was performed in the aim to evaluate nine different extracts from Tunisian Lycium arabicum for their total phenolic and total flavonoid contents, phytochemical analyses as well as their antioxidant and anti-lipase activities. The in vitro antioxidant property was investigated using three complementary methods (DPPH, ferric reducing antioxidant power (FRAP), and ß-carotene-linoleic acid bleaching assays) while anti-lipase activity was evaluated using 4-methylumbelliferyl oleate method. From all of the tested extracts the most potent found to be the polar MeOH extracts especially those of stems and leaves. In order to investigate the chemical composition of these extracts and possible correlation of their constituents with the observed activities, an UHPLC/HR-ESI-MS/MS analysis was performed. Several compounds belonging to different chemical classes were tentatively identified such as rutin and kampferol rutinoside, the major constituents of the leaves, and N-caffeoyltyramine, lyciumide A, N-dihydrocaffeoyltyramine as well as fatty acids: trihydroxyoctadecadienoic acid and hydroxyoctadecadienoic acid isomers were detected abundantly in the stems. These results showed that the MeOH extracts of stems and leaves of L. arabicum can be considered as a potential source of biological active compounds.
Assuntos
Antioxidantes/química , Inibidores Enzimáticos/química , Flavonoides/química , Lipase/antagonistas & inibidores , Lycium/química , Extratos Vegetais/química , Polifenóis/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Cromatografia Líquida de Alta Pressão , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Polifenóis/isolamento & purificação , Polifenóis/farmacologia , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em TandemRESUMO
CONTEXT: Despite some studies related to Juniperus phoenicea L. (Cupressaceae), phytochemical and biological investigations of this plant remain unexplored. OBJECTIVE: This work is the first report dealing with the identification and characterization of volatile components and flavonoids in hexane and methanol extracts from J. phoenicea leaves Materials and methods: Antioxidant activity of hexane, and methanol extracts from J. phoenicea leaves were determined by DPPH-radical scavenging assay. α-Amylase inhibitory activity was evaluated by enzyme inhibition using in vitro assay (each extract was dissolved in DMSO to give concentrations of 50, 100 and 200 mg/mL). The chemical composition of fractions (Fr1-Fr3) from methanol extract was determined by high-performance liquid chromatography coupled with mass spectroscopy (HPLC-MS) analysis. RESULTS AND DISCUSSION: The hexane extract was analyzed by GC-MS technique which allowed the identification of 32 compounds. The main constituents were α-humulene (16.9%), pentadecane (10.2%) and α-cubebene (9.7%). Fraction Fr 2 exhibited a strong DPPH radical-scavenging activity (IC50 = 20.1 µg/mL) compared to that of BHT as well as the highest α-amylase inhibitory activity (IC50 = 28.4 µg/mL). Three flavonoids were identified in these fractions using HPLC-MS analysis: Quercetin 3-O-glucoside, isoscutellarein 7-O-pentoside and quercetin 3-O-pentoside. In addition, the more active fraction (Fr 2) was purified with semi-preparative HPLC affording one pure compound (amentoflavone) using 1H NMR analysis. This compound exhibited powerful DPPH radical-scavenging (IC50 = 14.1 µg/mL) and α-amylase inhibition (IC50 = 20.4 µg/mL) effects. CONCLUSION: This study provides scientific support to some medicinal uses of J. phoenicea found in North Africa.
Assuntos
Cromatografia Líquida de Alta Pressão , Flavonoides/isolamento & purificação , Cromatografia Gasosa-Espectrometria de Massas , Juniperus/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Espectrometria de Massas em Tandem , Compostos Orgânicos Voláteis/isolamento & purificação , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Compostos de Bifenilo/química , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Flavonoides/farmacologia , Hexanos/química , Metanol/química , Fitoterapia , Picratos/química , Extratos Vegetais/farmacologia , Plantas Medicinais , Solventes/química , Tunísia , Compostos Orgânicos Voláteis/farmacologia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismoRESUMO
CONTEXT: Zygophyllum album L. (Zygophyllaceae), commonly known as Bougriba, is widely used to treat diabetes, digestive tract spasm, and hypertension in folk medicine, in Tunisia. OBJECTIVE: This study investigates the antidiabetic, antidiarrheal, and antihypertensive activities of the leaves of the essential oil from Zygophyllum album (OZA) in alloxan-induced diabetic rats. MATERIALS AND METHODS: The oil was obtained by hydrodistillation and analyzed by GC-MS. Males rats were divided into four groups: control, diabetic-untreated group, diabetic-treated group with acarbose (10 mg/kg), and diabetic-treated rats with OZA (200 mg/kg) for 30 d. RESULTS: At the end of the experimental period, the OZA significantly decreased the activity of α-amylase in pancreas and serum of the diabetic rats by 43% and 38%, respectively, which led to reduce the serum glucose level by 60% and lower of glycated hemoglobin (HbA1c) rate by 17% as compared with untreated diabetic animals. Moreover, the OZA treatment attenuated symptoms of diarrhea, improved lipid disorders, and hypertension through inhibiting the pancreatic lipase and angiotensin-converting enzyme (ACE) activities by 47% and 25%, respectively, in serum of diabetic rats. CONCLUSION: OZA showed a good effect in the management of diabetes mellitus and exerted preventive action from related hypertension.